盐酸替马沙星的新法合成
Novel Process for Preparation of Temafloxacin Hydrochloride
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摘要: 以2,4-二氯-5-氯苯甲酰乙酸乙酯为原料,经缩合、胺化,环合、螯合,取代,水解及成盐反应合成盐酸替马沙星。经元素分析,红外光谱,质谱和核磁共振谱确证结构,总收率45%。该工艺路线副反应少,产品纯度高。Abstract: In search for more reasonable process for preparation of polyfluorated quinolone antibacterial agents, temafloxacin hydrochloride is prepared from ethyl 2,4 dichloro 5 fluorobenzoylacetate, via condensation, amination, cyclization, boron esterification, substitution, hydrolysis and salt formation with 45% overall yield. The structure of temafloxacin hydrochloride is confirmed by MS, 1H NMR, IR and EA.